The present invention relates to piperidine derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their medical use.
In particular the invention relates to novel compounds which are potent and specific antagonists of tachykinins, including substance P and other neurokinins.
WO 97/16440 describes 1-(1,2-disubstituted piperidinyl)-4-substituted piperazine derivatives of general formula
wherein n and m are inter alia 1, p is 1; Q is inter alia oxygen; X is a covalent bond or a bivalent radical of formula —O—, —S—, NR3; R3 is hydrogen or a C1-6 alkyl group; R1 is inter alia Ar1; R2 may be inter alia Ar2C1-6alkyl wherein Ar2 and Ar1 are inter alia a phenyl group which may be substituted with 1, 2 or 3 substituents each independently selected from halo, C1-4alkyl, haloC1-4 alkyl, L may be inter alia hydrogen, C1-6 alkyl or L is a radical of formula —(CHR4)rC(O)Y1R7, wherein r is 0,1,2,3 or 4, Y1 is inter alia a NH or a N(C1-6 alkyl) group or Y1 is a covalent bond and R7 is inter alia C1-6 alkyl or C3-7 cycloalkyl. The compounds are antagonists of tachykinins.
We have now found a particular class of compounds which is not specifically disclosed therein, which class has special advantages.
We have discovered that by selection of particular substituents (namely a piperazin-1-yl substituent at the 4-position of the piperidine ring, substituted phenyl alkyl amide groups at the 1-position and substituted phenyl groups at the 2-position) a class of compounds having advantageous properties in the treatment of conditions mediated by tachykinins is obtained.